916484-09-8Relevant articles and documents
1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase
Lai, Mei-Jung,Ojha, Ritu,Lin, Mei-Hsiang,Liu, Yi-Min,Lee, Hsueh-Yun,Lin, Tony Eight,Hsu, Kai-Cheng,Chang, Chi-Yen,Chen, Mei-Chuan,Nepali, Kunal,Chang, Jang-Yang,Liou, Jing-Ping
, p. 612 - 630 (2019)
We report structure-activity relationships of 1-arylsulfonyl indoline based benzamides. The benzamide (9) exhibits striking tubulin inhibition with an IC50 value of 1.1 μM, better than that of combretastain A-4 (3), and substantial antiproliferative activity against a variety of cancer cells, including MDR-positive cell lines with an IC50 value of 49 nM (KB), 79 nM (A549), 63 nM (MKN45), 64 nM (KB-VIN10), 43 nM (KB-S15), and 46 nM (KB-7D). Dual inhibitory potential of compound 9 was found as it demonstrated significant inhibitory potential against HDAC1, 2 and 6 in comparison to MS-275 (6). Some key interactions of 9 with the amino acid residues of the active site of tubulin and with amino acid residues of HDAC 1 isoform have been figured out by molecular modeling. Compound 9 also demonstrated significant in vivo efficacy in the human non-small cell lung cancer A549 xenograft model as well as B-cell lymphoma BJAB xenograft tumor model.
Indoline-sulfonamides compounds
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Page/Page column 4, (2008/06/13)
A series of indoline-sulfonamide compounds is disclosed. The formula of indoline-sulfonamide compounds is shown as formula (I). In formula (I), R1 is H or halogen; R2 is Ar, Ar—C(O)—, Ar—CH2—, Ar—SO2—, Ar—O—C(O)
7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents
Chang, Jang-Yang,Hsieh, Hsing-Pang,Chang, Chi-Yen,Hsu, Kuo-Shun,Chiang, Yi-Fang,Chen, Chi-Ming,Kuo, Ching-Chuan,Liou, Jing-Ping
, p. 6656 - 6659 (2008/04/18)
A novel series of 7-aroyl-aminoindoline-1-benzenesulfonamides showed excellent activity as inhibitors of tubulin polymerization through binding with the colchicine binding site of microtubules. Compound 15 and 16 display IC 50 values of 1.1 and