PMID- 20930398 OWN - NLM STAT- MEDLINE DCOM- 20110202 LR - 20190706 IS - 1347-5223 (Electronic) IS - 0009-2363 (Linking) VI - 58 IP - 10 DP - 2010 Oct TI - Synthesis, cytotoxicity and pro-apoptosis of novel benzoisoindolin hydrazones as anticancer agents. PG - 1324-7 AB - A series of benzoisoindolin hydrazones as analogues of natural lignan diphyllin were synthesized and the structures of these compounds were established by (1)H-NMR, (13)C-NMR, Mass and high resolution (HR)-MS. The compounds were evaluated for in vitro cytotoxicity against KB, A549 and HCT-116 cancer cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Compound 4 possessed the highest growth inhibitory effect. Significant apoptosis of HCT-116 cells treated with compound 4 was observed by Hoechst33342-propidium iodide (PI) and acridine orange (AO)-ethidium bromide (EB) staining assay. Western blot analysis disclosed that compound 4 induced apoptosis via the mitochondrial pathway accompanied by an increased expression of Bax and a decreased expression of Bcl-2. FAU - Zhao, Yu AU - Zhao Y AD - Institute of Nautical Medicine, Nantong University, People's Republic of China. FAU - Hui, Jie AU - Hui J FAU - Wang, Dan AU - Wang D FAU - Zhu, Li AU - Zhu L FAU - Fang, Jing-Huai AU - Fang JH FAU - Zhao, Xiao-Dong AU - Zhao XD LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Japan TA - Chem Pharm Bull (Tokyo) JT - Chemical & pharmaceutical bulletin JID - 0377775 RN - 0 (Antineoplastic Agents) RN - 0 (Hydrazones) RN - 0 (Indoles) RN - 0 (Isoindoles) RN - 0 (N-(4-methylbenzylidenyl)-4'-(3'',4''-methylenedioxyphenyl)-6',7'- dimethoxyl-1'-hydroxyl-benzyl-2,3-dihydro-isoindol-1-hydrazone) RN - 0 (Proto-Oncogene Proteins c-bcl-2) RN - 0 (bcl-2-Associated X Protein) RN - 6DPT9AB2NK (indoline) SB - IM MH - Antineoplastic Agents/*chemical synthesis/therapeutic use/toxicity MH - *Apoptosis MH - Cell Line, Tumor MH - Humans MH - Hydrazones/chemical synthesis/*chemistry/therapeutic use/toxicity MH - Indoles/*chemistry MH - Isoindoles/chemical synthesis/therapeutic use/toxicity MH - Mitochondria/metabolism MH - Neoplasms/drug therapy MH - Proto-Oncogene Proteins c-bcl-2/metabolism MH - bcl-2-Associated X Protein/metabolism EDAT- 2010/10/12 06:00 MHDA- 2011/02/03 06:00 CRDT- 2010/10/09 06:00 PHST- 2010/10/09 06:00 [entrez] PHST- 2010/10/12 06:00 [pubmed] PHST- 2011/02/03 06:00 [medline] AID - JST.JSTAGE/cpb/58.1324 [pii] AID - 10.1248/cpb.58.1324 [doi] PST - ppublish SO - Chem Pharm Bull (Tokyo). 2010 Oct;58(10):1324-7. doi: 10.1248/cpb.58.1324.