REFERENCES
1. Sung H, Ferlay J, Siegel RL, et al. Global Cancer Statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. CA Cancer J Clin. 2021;71:209-49.
2. Wang Q, Shen X, Chen G, Du J. Drug resistance in colorectal cancer: from mechanism to clinic. Cancers. 2022;14:2928.
3. Therachiyil L, Haroon J, Sahir F, et al. Dysregulated phosphorylation of p53, autophagy and stemness attributes the mutant p53 harboring colon cancer cells impaired sensitivity to oxaliplatin. Front Oncol. 2020;10:1744.
4. Grassilli E, Cerrito MG. Emerging actionable targets to treat therapy-resistant colorectal cancers. Cancer Drug Resist. 2022;5:36-63.
5. Rainho MA, Siqueira PB, de Amorim ÍSS, Mencalha AL, Thole AA. Mitochondria in colorectal cancer stem cells - a target in drug resistance. Cancer Drug Resist. 2023;6:273-83.
6. Shi Z, Fultz RS, Engevik MA, et al. Distinct roles of histamine H1- and H2-receptor signaling pathways in inflammation-associated colonic tumorigenesis. Am J Physiol Gastrointest Liver Physiol. 2019;316:G205-16.
7. Zhao J, Hou Y, Yin C, et al. Upregulation of histamine receptor H1 promotes tumor progression and contributes to poor prognosis in hepatocellular carcinoma. Oncogene. 2020;39:1724-38.
8. Li H, Xiao Y, Li Q, et al. The allergy mediator histamine confers resistance to immunotherapy in cancer patients via activation of the macrophage histamine receptor H1. Cancer Cell. 2022;40:36-52.e9.
9. Zhong P, Nakata K, Oyama K, et al. Blockade of histamine receptor H1 augments immune checkpoint therapy by enhancing MHC-I expression in pancreatic cancer cells. J Exp Clin Cancer Res. 2024;43:138.
10. Borowy CS, Mukherji P. Antihistamine toxicity. Treasure Island (FL): StatPearls Publishing; 2023.
11. Vitaku E, Smith DT, Njardarson JT. Analysis of the structural diversity, substitution patterns, and frequency of nitrogen heterocycles among U.S. FDA approved pharmaceuticals. J Med Chem. 2014;57:10257-74.
12. Zhang Y, Wu C, Zhang N, Fan R, Ye Y, Xu J. Recent advances in the development of pyrazole derivatives as anticancer agents. Int J Mol Sci. 2023;24:12724.
13. Matiadis D, Sagnou M. Pyrazoline hybrids as promising anticancer agents: an up-to-date overview. Int J Mol Sci. 2020;21:5507.
14. Yusuf M, Jain P. Synthetic and biological studies of pyrazolines and related heterocyclic compounds. Arab J Chem. 2014;7:553-96.
15. Farooq S, Ngaini Z. One-pot and two-pot synthesis of chalcone based mono and bis-pyrazolines. Tetrahedron Lett. 2020;61:151416.
16. Nepali K, Kadian K, Ojha R, et al. Effect of ring A and ring B substitution on the cytotoxic potential of pyrazole tethered chalcones. Med Chem Res. 2012;21:2990-7.
17. Padhye S, Ahmad A, Oswal N, et al. Fluorinated 2’-hydroxychalcones as garcinol analogs with enhanced antioxidant and anticancer activities. Bioorg Med Chem Lett. 2010;20:5818-21.
18. Singh P, Negi JS, Pant GJN, Rawat MSM. Synthesis and characterization of novel 1-chloroacetyl derivatives of 2-pyrazolines. Heterocycl Commun. 2011;17:61-3.
19. Divekar K, Swamy S, Kavitha N, Murugan V, Devgun M. Synthesis and evaluation of some new pyrazole derivatives as antimicrobial agents. Res J Pharm Technol. 2010;3:1039-43.
20. Gervaz P, Fontolliet C. Therapeutic potential of the anti-angiogenesis drug TNP-470. Int J Exp Pathol. 1998;79:359-62.
21. Shushan A, Ben-Bassat H, Mishani E, Laufer N, Klein BY, Rojansky N. Inhibition of leiomyoma cell proliferation in vitro by genistein and the protein tyrosine kinase inhibitor TKS050. Fertil Steril. 2007;87:127-35.
22. Fumarola C, Bozza N, Castelli R, et al. Expanding the arsenal of FGFR inhibitors: a novel chloroacetamide derivative as a new irreversible agent with anti-proliferative activity against FGFR1-amplified lung cancer cell lines. Front Oncol. 2019;9:179.
23. Ramkumar K, Samanta S, Kyani A, et al. Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor. Nat Commun. 2016;7:13084.
24. Tsuboi K, Bachovchin DA, Speers AE, et al. Potent and selective inhibitors of glutathione S-transferase omega 1 that impair cancer drug resistance. J Am Chem Soc. 2011;133:16605-16.
25. Randolph JT, O’Connor MJ, Han F, et al. Discovery of a potent chloroacetamide GPX4 inhibitor with bioavailability to enable target engagement in mice, a potential tool compound for inducing ferroptosis in vivo. J Med Chem. 2023;66:3852-65.
26. Lee HY, Suciu RM, Horning BD, Vinogradova EV, Ulanovskaya OA, Cravatt BF. Covalent inhibitors of nicotinamide N-methyltransferase (NNMT) provide evidence for target engagement challenges in situ. Bioorg Med Chem Lett. 2018;28:2682-7.
27. Zhang P, Tao H, Yu L, Zhou L, Zhu C. Developing protein arginine methyltransferase 1 (PRMT1) inhibitor TC-E-5003 as an antitumor drug using INEI drug delivery systems. Drug Deliv. 2020;27:491-501.
28. Kim E, Jang J, Park JG, et al. Protein arginine methyltransferase 1 (PRMT1) selective inhibitor, TC-E 5003, has anti-inflammatory properties in TLR4 signaling. Int J Mol Sci. 2020;21:3058.
29. Anchoori RK, Tan M, Tseng SH, et al. Structure-function analyses of candidate small molecule RPN13 inhibitors with antitumor properties. PLoS One. 2020;15:e0227727.
30. Cogoi S, Zorzet S, Shchekotikhin AE, Xodo LE. Potent apoptotic response induced by chloroacetamidine anthrathiophenediones in bladder cancer cells. J Med Chem. 2015;58:5476-85.
31. Makar S, Saha T, Singh SK. Naphthalene, a versatile platform in medicinal chemistry: sky-high perspective. Eur J Med Chem. 2019;161:252-76.
32. Schmitt F, Draut H, Biersack B, Schobert R. Halogenated naphthochalcones and structurally related naphthopyrazolines with antitumor activity. Bioorg Med Chem Lett. 2016;26:5168-71.
33. Ethiraj KR, Nithya P, Krishnakumar V, Jesil Mathew A, Nawaz Khan F. Synthesis and cytotoxicity study of pyrazoline derivatives of methoxy substituted naphthyl chalcones. Res Chem Intermed. 2013;39:1833-41.
34. Sánchez Maya AB, Pérez-Melero C, Salvador N, Peláez R, Caballero E, Medarde M. New naphthylcombretastatins. Modifications on the ethylene bridge. Bioorg Med Chem. 2005;13:2097-107.
35. Ornelas C, Astruc D. Ferrocene-based drugs, delivery nanomaterials and fenton mechanism: state of the art, recent developments and prospects. Pharmaceutics. 2023;15:2044.
36. Li L, Ma L, Sun J. The antiproliferative activity of ferrocene derivatives against drug- resistant cancer cell lines: a mini review. Curr Top Med Chem. 2021;21:1756-72.
37. Wu X, Tiekink ER, Kostetski I, et al. Antiplasmodial activity of ferrocenyl chalcones: investigations into the role of ferrocene. Eur J Pharm Sci. 2006;27:175-87.
38. Spencer J, Amin J, Wang M, et al. Synthesis and biological evaluation of JAHAs: ferrocene-based histone deacetylase inhibitors. ACS Med Chem Lett. 2011;2:358-62.
39. Philipova I, Mihaylova R, Momekov G, Angelova R, Stavrakov G. Ferrocene modified analogues of imatinib and nilotinib as potent anti-cancer agents. RSC Med Chem. 2023;14:880-9.
40. Wu X, Wilairat P, Go ML. Antimalarial activity of ferrocenyl chalcones. Bioorg Med Chem Lett. 2002;12:2299-302.
41. Harkov S, Havrylyuk D, Atamanyuk V, Zimenkovsky B, Lesyk R. Synthesis and biological activity of isatines bearing thiazolidinone and pyrazoline moieties. Pharmacia. 2013;60:8-18. Available from: https://www.researchgate.net/publication/287329904_Synthesis_and_biological_activity_of_isatines_bearing_thiazolidinone_and_pyrazoline_moieties. [Last accessed on 8 Apr 2026].
42. Dandawate P, Vemuri K, Khan EM, Sritharan M, Padhye S. Synthesis, characterization and anti-tubercular activity of ferrocenyl hydrazones and their β-cyclodextrin conjugates. Carbohydr Polym. 2014;108:135-44.
43. Ma J, Veeragoni D, Ghosh H, et al. Superior anticancer and antifungal activities of new sulfanyl-substituted niclosamide derivatives. Biomedicines. 2024;12:1621.
44. Chen X, Liao Y, Long D, Yu T, Shen F, Lin X. The Cdc2/Cdk1 inhibitor, purvalanol A, enhances the cytotoxic effects of taxol through Op18/stathmin in non-small cell lung cancer cells in vitro. Int J Mol Med. 2017;40:235-42.
45. Ghosh H, Bhattacharyya S, Schobert R, Dandawate P, Biersack B. Fluorinated and N-acryloyl-modified 3,5-Di[(E)-benzylidene]piperidin-4-one curcuminoids for the treatment of pancreatic carcinoma. Pharmaceutics. 2023;15:1921.
46. Landegren U. Measurement of cell numbers by means of the endogenous enzyme hexosaminidase. Applications to detection of lymphokines and cell surface antigens. J Immunol Methods. 1984;67:379-88.
47. Oberhuber N, Ghosh H, Nitzsche B, et al. Synthesis and anticancer evaluation of new indole-based tyrphostin derivatives and their (p-cymene)dichloridoruthenium(II) complexes. Int J Mol Sci. 2023;24:854.
48. Ianevski A, Giri AK, Aittokallio T. SynergyFinder 3.0: an interactive analysis and consensus interpretation of multi-drug synergies across multiple samples. Nucleic Acids Res. 2022;50:W739-43.
49. Ianevski A, Giri AK, Gautam P, et al. Prediction of drug combination effects with a minimal set of experiments. Nat Mach Intell. 2019;1:568-77.
50. Dandawate P, Subramaniam D, Panovich P, et al. Cucurbitacin B and I inhibits colon cancer growth by targeting the Notch signaling pathway. Sci Rep. 2020;10:1290.
51. Franken NA, Rodermond HM, Stap J, Haveman J, van Bree C. Clonogenic assay of cells in vitro. Nat Protoc. 2006;1:2315-9.
52. Bhattacharyya S, Ghosh H, Covarrubias-Zambrano O, et al. Anticancer activity of novel difluorinated curcumin analog and its inclusion complex with 2-hydroxypropyl-β-cyclodextrin against pancreatic cancer. Int J Mol Sci. 2023;24:6336.
53. Dandawate P, Kaushik G, Ghosh C, et al. Diphenylbutylpiperidine antipsychotic drugs inhibit prolactin receptor signaling to reduce growth of pancreatic ductal adenocarcinoma in mice. Gastroenterology. 2020;158:1433-49.e27.
54. Schleser SW, Ghosh H, Hörner G, et al. New 4,5-diarylimidazol-2-ylidene-iodidogold(I) complexes with high activity against esophageal adenocarcinoma cells. Int J Mol Sci. 2023;24:5738.
55. Shimamura T, Shiroishi M, Weyand S, et al. Structure of the human histamine H1 receptor complex with doxepin. Nature. 2011;475:65-70.
56. Trott O, Olson AJ. AutoDock Vina: improving the speed and accuracy of docking with a new scoring function, efficient optimization, and multithreading. J Comput Chem. 2010;31:455-61.
57. Alexander N, Woetzel N, Meiler J. bcl::Cluster : a method for clustering biological molecules coupled with visualization in the Pymol Molecular Graphics System. IEEE Int Conf Comput Adv Bio Med Sci. 2011:13-8.
58. Jafari R, Almqvist H, Axelsson H, et al. The cellular thermal shift assay for evaluating drug target interactions in cells. Nat Protoc. 2014;9:2100-22.
59. Krishnamachary B, Subramaniam D, Dandawate P, et al. Targeting transcription factor TCF4 by γ-Mangostin, a natural xanthone. Oncotarget. 2019;10:5576-91.
60. Altıntop MD, Cantürk Z, Özdemir A. Design, synthesis, and evaluation of a new series of 2-pyrazolines as potential antileukemic agents. ACS Omega. 2023;8:42867-77.
61. Hientz K, Mohr A, Bhakta-Guha D, Efferth T. The role of p53 in cancer drug resistance and targeted chemotherapy. Oncotarget. 2017;8:8921-46.
62. Pardini B, Kumar R, Naccarati A, et al. 5-Fluorouracil-based chemotherapy for colorectal cancer and MTHFR/MTRR genotypes. Br J Clin Pharmacol. 2011;72:162-3.
63. Lee EF, Harris TJ, Tran S, et al. BCL-XL and MCL-1 are the key BCL-2 family proteins in melanoma cell survival. Cell Death Dis. 2019;10:342.
64. Zanoni M, Piccinini F, Arienti C, et al. 3D tumor spheroid models for in vitro therapeutic screening: a systematic approach to enhance the biological relevance of data obtained. Sci Rep. 2016;6:19103.
65. Goldman MJ, Craft B, Hastie M, et al. Visualizing and interpreting cancer genomics data via the Xena platform. Nat Biotechnol. 2020;38:675-8.
66. Jain R, Watson U, Saini DK. ERK activated by Histamine H1 receptor is anti-proliferative through spatial restriction in the cytosol. Eur J Cell Biol. 2016;95:623-34.
67. Diks SH, Hardwick JC, Diab RM, et al. Activation of the canonical beta-catenin pathway by histamine. J Biol Chem. 2003;278:52491-6.
68. Miller I, Min M, Yang C, et al. Ki67 is a graded rather than a binary marker of proliferation versus quiescence. Cell Rep. 2018;24:1105-12.e5.
69. Chu XY, Suzuki H, Ueda K, Kato Y, Akiyama S, Sugiyama Y. Active efflux of CPT-11 and its metabolites in human KB-derived cell lines. J Pharmacol Exp Ther. 1999;288:735-41.
70. Matsunaga T, Okumura N, Saito H, et al. Significance of aldo-keto reductase 1C3 and ATP-binding cassette transporter B1 in gain of irinotecan resistance in colon cancer cells. Chem Biol Interact. 2020;332:109295.
71. Chu X, Tian W, Ning J, et al. Cancer stem cells: advances in knowledge and implications for cancer therapy. Signal Transduct Target Ther. 2024;9:170.
72. Zhou Y, Xia L, Wang H, et al. Cancer stem cells in progression of colorectal cancer. Oncotarget. 2018;9:33403-15.
73. Chai Y, Liu JL, Zhang S, et al. The effective combination therapies with irinotecan for colorectal cancer. Front Pharmacol. 2024;15:1356708.
75. Niu Y, Sun W, Lu JJ, et al. PTEN activation by DNA damage induces protective autophagy in response to cucurbitacin B in hepatocellular carcinoma cells. Oxid Med Cell Longev. 2016;2016:4313204.
76. Zeng L, Tang M, Pi C, et al. Novel ferrocene derivatives induce apoptosis through mitochondria-dependent and cell cycle arrest via PI3K/Akt/mTOR signaling pathway in T cell acute lymphoblastic leukemia. Cancers. 2021;13:4677.
77. Choudhary GS, Al-Harbi S, Mazumder S, et al. MCL-1 and BCL-xL-dependent resistance to the BCL-2 inhibitor ABT-199 can be overcome by preventing PI3K/AKT/mTOR activation in lymphoid malignancies. Cell Death Dis. 2015;6:e1593.
78. Jun SY, Kim J, Yoon N, Maeng LS, Byun JH. Prognostic potential of cyclin D1 expression in colorectal cancer. J Clin Med. 2023;12:572.
79. Montalto FI, De Amicis F. Cyclin D1 in cancer: a molecular connection for cell cycle control, adhesion and invasion in tumor and stroma. Cells. 2020;9:2648.
80. Guo J, Zhou AW, Fu YC, et al. Efficacy of sequential treatment of HCT116 colon cancer monolayers and xenografts with docetaxel, flavopiridol, and 5-fluorouracil. Acta Pharmacol Sin. 2006;27:1375-81.
81. Jung J. Human tumor xenograft models for preclinical assessment of anticancer drug development. Toxicol Res. 2014;30:1-5.
82. Lazebnik YA, Kaufmann SH, Desnoyers S, Poirier GG, Earnshaw WC. Cleavage of poly(ADP-ribose) polymerase by a proteinase with properties like ICE. Nature. 1994;371:346-7.
