TY - JOUR
T1 - Recent developments on phenstatins as potent antimitotic agents
AU - Chen, Xing
AU - Wang, Shi Meng
AU - Kumar, Gajjela Bharath
AU - Bare, Grant A.L.
AU - Leng, Jing
AU - Bukhari, Syed Nasir Abbas
AU - Qin, Hua Li
N1 - Publisher Copyright:
© 2018 Bentham Science Publishers.
PY - 2018
Y1 - 2018
N2 - Background: Phenstatin and their derivatives display remarkable antiproliferative activity toward a wide variety of preclinical tumor models. Structural simplicity and excellent stability of phenstatins offer a stimulating premise for developing various derivatives with profound antimitotic activity and excellent cytotoxicity. Objective: To do analysis of literature that phenstatins derivatives inhibit tubulin polymerization through their interaction at the colchicine binding site of microtubules and arrest the G2/M phase of the cell cycle. In addition, phenstatin derivatives are undergoing clinical evaluation as vascular targeting/disrupting agents and also exhibit direct antiangiogenic properties. Methods: An organised well designed and appropriately managed search of bibliographic databases for peer-reviewed research literature using a focused review question and inclusion/ exclusion criteria has been done for this article. Conclusion: In this review article, the synthesis and structure-activity relationships of phenstatin and a wide number of their reported analogues with modifications to ring A, ring B, and to the keto position are discussed in the perspective of medicinal chemistry with proper conclusion.
AB - Background: Phenstatin and their derivatives display remarkable antiproliferative activity toward a wide variety of preclinical tumor models. Structural simplicity and excellent stability of phenstatins offer a stimulating premise for developing various derivatives with profound antimitotic activity and excellent cytotoxicity. Objective: To do analysis of literature that phenstatins derivatives inhibit tubulin polymerization through their interaction at the colchicine binding site of microtubules and arrest the G2/M phase of the cell cycle. In addition, phenstatin derivatives are undergoing clinical evaluation as vascular targeting/disrupting agents and also exhibit direct antiangiogenic properties. Methods: An organised well designed and appropriately managed search of bibliographic databases for peer-reviewed research literature using a focused review question and inclusion/ exclusion criteria has been done for this article. Conclusion: In this review article, the synthesis and structure-activity relationships of phenstatin and a wide number of their reported analogues with modifications to ring A, ring B, and to the keto position are discussed in the perspective of medicinal chemistry with proper conclusion.
KW - Antimitotic activity
KW - Colchicine binding site
KW - Cytotoxic activity
KW - Phenstatins
KW - Structure-activity relationship
KW - Tubulin polymerization inhibition
UR - https://www.scopus.com/pages/publications/85048867986
U2 - 10.2174/0929867324666171106162048
DO - 10.2174/0929867324666171106162048
M3 - Review article
C2 - 29110592
AN - SCOPUS:85048867986
SN - 0929-8673
VL - 25
SP - 2329
EP - 2352
JO - Current Medicinal Chemistry
JF - Current Medicinal Chemistry
IS - 20
ER -