Abstract
Tubulin inhibitors can interfere with normal cell mitosis and inhibit cell proliferation through interfering with the normal structure and function of microtubules, forming spindle filaments. Indole, as a privileged pharmacological skeleton, has been widely used in anti-cancer inhibitors. A variety of alkaloids containing an indole core obtained from natural sources have been proven to inhibit tubulin polymerization, and an ever-increasing number of synthetic indole-based tubulin inhibitors have been reported. Among these, several kinds of indole-based derivatives, such as TMP analogues, aroylindoles, arylthioindoles, fused indole, carbazoles, azacarbolines, alkaloid nortopsentin analogues and bis-indole derivatives, have shown good inhibition activities towards tubulin polymerization. The binding modes and SARs investigations of synthetic indole derivatives, along with a brief mechanism on their anti-tubulin activity, are presented in this review.
Highlights
Cancer, a multifaceted, multi-mechanistic and life-threatening disease, is one of the appalling scourges worldwide
Cancer cells are characterized by uncontrollable proliferation, unstoppable differentiation and unpredictable migration [1–3]
Several indole derivatives have been provided as a versatile pharmacological structure in drug modification. These derivatives have been widely used in target-based anti-cancer inhibitors, and some of which have been approved by the FDA (Table 1)
Summary
A multifaceted, multi-mechanistic and life-threatening disease, is one of the appalling scourges worldwide. Several indole derivatives have been provided as a versatile pharmacological structure in drug modification These derivatives have been widely used in target-based anti-cancer inhibitors, and some of which have been approved by the FDA (Table 1). Vincristine, a tubulin drug, is an anti-tumor alkaloid roseus, which inhibits microtubule formation in the mitotic spindle and leads to splinter. As a of vincristine has a hydrogen bond interaction with ASN329 and a π-σ conjugation wi core pharmacophore, the indole scaffold served a crucially important role in interacting. The indole scaffold served a crucially im with the colchicine binding site (Col, violet), which has a small cavity volume and is easier portant role in interacting with the colchicine binding site (Col, violet), which has a sma to modify. On the colchicine bindingofsite of tub indole-derived lin compounds in application the design of anticancer agents.
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