TY - JOUR
T1 - Design, synthesis and biological evaluation of novel 1,5-disubstituted isatin derivatives as antitumor agents
AU - Zhuo, Huijun
AU - Zhang, Zhen
AU - Liu, Yang
AU - Zhang, Jingya
AU - Zhao, Guisen
N1 - Publisher Copyright:
© 2020, Springer Science+Business Media, LLC, part of Springer Nature.
PY - 2020/12/1
Y1 - 2020/12/1
N2 - Isatin (1H-indole-2,3-dione) was reported to possess anticancer activities through its effect on tumor proliferation, apoptosis, and metastasis in vitro and in vivo. Here, we described the synthesis of a novel series of 1,5-disubstituted isatin derivatives with 2-indolinone scaffold as antitumor agents. Most of the synthesized compounds revealed potent antiproliferative effects in mantle cell lymphoma (MCL) cell lines, among which 7l possessed promising activities with IC50 values ranging from 0.4 to 1.3 μM. Following flow cytometric analysis, compound 7l efficiently arrested the cell cycle at G2/M phase, and induced apoptosis. Thus, this study shows promise in therapeutics of 1,5-disubstituted isatin derivatives in MCL and provides novel potential and efficient antitumor agents. [Figure not available: see fulltext.]
AB - Isatin (1H-indole-2,3-dione) was reported to possess anticancer activities through its effect on tumor proliferation, apoptosis, and metastasis in vitro and in vivo. Here, we described the synthesis of a novel series of 1,5-disubstituted isatin derivatives with 2-indolinone scaffold as antitumor agents. Most of the synthesized compounds revealed potent antiproliferative effects in mantle cell lymphoma (MCL) cell lines, among which 7l possessed promising activities with IC50 values ranging from 0.4 to 1.3 μM. Following flow cytometric analysis, compound 7l efficiently arrested the cell cycle at G2/M phase, and induced apoptosis. Thus, this study shows promise in therapeutics of 1,5-disubstituted isatin derivatives in MCL and provides novel potential and efficient antitumor agents. [Figure not available: see fulltext.]
KW - Antitumor
KW - Apoptosis
KW - Isatin derivatives
KW - Mantle cell lymphoma
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U2 - 10.1007/s00044-020-02627-z
DO - 10.1007/s00044-020-02627-z
M3 - Article
AN - SCOPUS:85091356265
SN - 1054-2523
VL - 29
SP - 2170
EP - 2180
JO - Medicinal Chemistry Research
JF - Medicinal Chemistry Research
IS - 12
ER -