Development of hydrazide hydrazone-tethered combretastatin-oxindole derivatives as antimitotic agents

Bora, Darshana; Sharma, Anamika; John, Stephy Elza; Shankaraiah, Nagula

doi:10.1016/j.molstruc.2022.134675

Cited by 1 publication

(1 citation statement)

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“…[120] Isatin-combretastatin hybrid 79 (IC 50 : 3.49 µM) was not inferior to colchicine (IC 50 : 3.30 µM) and combretastatin A-4 (IC 50 : 9.31 µM) against MCF-7 cells and exhibited low cytotoxicity (IC 50 : 43.61 µM) against normal HaCaT cells. [121] Mechanistically, hybrid 79 might stimulate the formation of ROS, and consequently, ROS-mediated cell death and apoptosis process modulation. In addition, hybrid 79 suppressed tubulin polymerization and arrested the cell cycle during the G2/M phase.…”

Section: Miscellaneous Indole/isatin Hybridsmentioning

confidence: 99%

The anti‐breast cancer potential of indole/isatin hybrids

Wang,

Huang,

Yuan

et al. 2023

Archiv der Pharmazie

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Breast cancer (BC) is one of the most prevalent malignancies and the major contributor to cancer mortality in women globally, with a high degree of heterogeneity and a dismal prognosis. As drug resistance is responsible for most BC fatalities and advanced BC is currently considered incurable, finding innovative anti‐BC chemotherapeutics is urgently required. Indole and its analog isatin (indole‐1H‐2,3‐dione) are prominent pharmacophores in the development of novel medications, and their derivatives exhibit strong anticancer activities, also against BC. In particular, indole/isatin hybrids exhibit significant potency against BC including multidrug‐resistant forms and excellent selectivity by influencing a variety of biological targets associated with the disease, supplying helpful building blocks for the identification of potential new BC treatment options. This review includes articles from 2020 to the present and provides insights into the in vitro and in vivo anti‐BC potential, molecular mechanisms, and structure–activity relationships (SARs) of indole/isatin hybrids that may be helpful in the development of innovative anti‐BC chemotherapeutics.

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Section: Miscellaneous Indole/isatin Hybridsmentioning

confidence: 99%