Bioorganic and Medicinal Chemistry Letters, volume 27, issue 2, pages 261-265
Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility
Publication type: Journal Article
Publication date: 2017-01-01
Quartile SCImago
Q2
Quartile WOS
Q2
Impact factor: 2.7
ISSN: 0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
The current optimization of IG-105 (3) on the carbazole-ring provided a series of new carbazole sulfonamides derivatives 13a-13m. All of the compounds have been evaluated against HepG2 cells (hepatoma cancer) for antiproliferative activity. Compounds that showed activity better or comparable to that of 3 versus HepG2 were evaluated against MCF-7 (breast cancer), MIA PaCa-2 (pancreatic cancer), and Bel-7402 (hepatoma/liver cancer) for antiproliferative activity. Of the seven compounds selected for further study five (13b, 13g, 13j, 13k and 13l) were found to give IC50 values against the four cell lines comparable to those for 3. Two compounds (13f and 13i) were more active than 3 and their activity against HepG2 and MCF-7 (IC50:0.01-0.07μM) approached that of the positive controls podophyllotoxin (podo) and CA-4. Most of compounds showed aqueous solubility (0.11-19.60μg/mL at pH 7.4 and 2.0) better than 3. These promising results warrant further development of new compounds 13f and 13i as potential potent antitumor drug candidates.
Citations by journals
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1 publication, 3.7%
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Citations by publishers
2
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10
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10 publications, 37.04%
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4 publications, 14.81%
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2 publications, 7.41%
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2 publications, 7.41%
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American Chemical Society (ACS)
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2 publications, 7.41%
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Pleiades Publishing
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Pleiades Publishing
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Taylor & Francis
2 publications, 7.41%
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Frontiers Media S.A.
1 publication, 3.7%
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Thieme
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Thieme
1 publication, 3.7%
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Future Medicine
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Future Medicine
1 publication, 3.7%
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4
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10
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- We do not take into account publications that without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
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Sun L. et al. Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility // Bioorganic and Medicinal Chemistry Letters. 2017. Vol. 27. No. 2. pp. 261-265.
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Sun L., Wu Y., Liu Y., Chen X., Hu L. Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility // Bioorganic and Medicinal Chemistry Letters. 2017. Vol. 27. No. 2. pp. 261-265.
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TY - JOUR
DO - 10.1016/j.bmcl.2016.11.068
UR - https://doi.org/10.1016%2Fj.bmcl.2016.11.068
TI - Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Sun, Lianqi
AU - Wu, Yanbin
AU - Liu, Yonghua
AU - Chen, Xiaofang
AU - Hu, Laixing
PY - 2017
DA - 2017/01/01 00:00:00
PB - Elsevier
SP - 261-265
IS - 2
VL - 27
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2017_Sun,
author = {Lianqi Sun and Yanbin Wu and Yonghua Liu and Xiaofang Chen and Laixing Hu},
title = {Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2017},
volume = {27},
publisher = {Elsevier},
month = {jan},
url = {https://doi.org/10.1016%2Fj.bmcl.2016.11.068},
number = {2},
pages = {261--265},
doi = {10.1016/j.bmcl.2016.11.068}
}
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Sun, Lianqi, et al. “Novel carbazole sulfonamide derivatives of antitumor agent: Synthesis, antiproliferative activity and aqueous solubility.” Bioorganic and Medicinal Chemistry Letters, vol. 27, no. 2, Jan. 2017, pp. 261-265. https://doi.org/10.1016%2Fj.bmcl.2016.11.068.