PMID- 22897207 OWN - NLM STAT- MEDLINE DCOM- 20121226 LR - 20240322 IS - 2159-3345 (Electronic) IS - 2159-3337 (Print) IS - 2159-3337 (Linking) VI - 22 IP - 4 DP - 2012 Aug TI - Antiproliferative activity of novel thiopyran analogs on MCF-7 breast and HCT-15 colon cancer cells: synthesis, cytotoxicity, cell cycle analysis, and DNA-binding. PG - 265-70 LID - 10.1089/nat.2012.0346 [doi] AB - A series of 6H-thiopyran-2,3-dicarboxylate derivatives 4a-d were synthesized and evaluated for their cytotoxic effect against HCT-15 colon and MCF-7 breast cancer cell lines using Sulforhodamine B (SRB) assay. The results showed that these compounds could exhibit a good cytotoxicity to both cell lines. In addition, these compounds were found to exhibit significant DNA-binding affinity. Ultraviolet-visible light (UV-Vis) spectroscopy was conducted to determine the ability of the ligand under analysis. The effect of ligand complexation on DNA structure led to overall affinity constants of K(4a)=3.5x10(4) M(-1), K(4b)=6.4x10(4) M(-1), K(4c)=3.2x10(4) M(-1), and K(4d)=2.4x10(4) M(-1). Our findings could provide new evidence showing the relationship between the chemical structure and biological activity and may be useful for the discovery of new anti-cancer drugs. FAU - Tavakolinia, Fatemeh AU - Tavakolinia F AD - Department of Chemistry, University of Canterbury, Christchurch, New Zealand. FAU - Baghipour, Tayebeh AU - Baghipour T FAU - Hossaini, Zinatossadat AU - Hossaini Z FAU - Zareyee, Daryoush AU - Zareyee D FAU - Khalilzadeh, Mohammad A AU - Khalilzadeh MA FAU - Rajabi, Mehdi AU - Rajabi M LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20120816 PL - United States TA - Nucleic Acid Ther JT - Nucleic acid therapeutics JID - 101562758 RN - 0 (Antineoplastic Agents) RN - 0 (Pyrans) RN - 0 (Sulfhydryl Compounds) RN - 9007-49-2 (DNA) SB - IM MH - Antineoplastic Agents/chemical synthesis/chemistry/*pharmacology MH - Apoptosis/drug effects MH - Breast Neoplasms MH - Cell Cycle/*drug effects MH - Cell Line, Tumor MH - Cell Proliferation/*drug effects MH - Cell Shape/drug effects MH - Colonic Neoplasms MH - DNA/*chemistry MH - Drug Screening Assays, Antitumor MH - Female MH - Humans MH - Inhibitory Concentration 50 MH - Pyrans/chemical synthesis/chemistry/*pharmacology MH - Sulfhydryl Compounds/chemical synthesis/chemistry/*pharmacology PMC - PMC3426206 EDAT- 2012/08/18 06:00 MHDA- 2012/12/27 06:00 PMCR- 2012/08/01 CRDT- 2012/08/18 06:00 PHST- 2012/08/18 06:00 [entrez] PHST- 2012/08/18 06:00 [pubmed] PHST- 2012/12/27 06:00 [medline] PHST- 2012/08/01 00:00 [pmc-release] AID - 10.1089/nat.2012.0346 [pii] AID - 10.1089/nat.2012.0346 [doi] PST - ppublish SO - Nucleic Acid Ther. 2012 Aug;22(4):265-70. doi: 10.1089/nat.2012.0346. Epub 2012 Aug 16.