1,3,4‐oxadiazole and its derivatives: A review on recent progress in anticancer activities

Abstract

The 1,3,4-oxadiazole nucleus is a biologically imperative scaffold possesses numerous biological activities. The broad and potent activity of 1,3,4-oxadiazole and their derivatives has established them as important pharmacological scaffolds especially in the treatment of cancer disease. Several di-, tri-, aromatic, and heterocyclic substituted 1,3,4-oxadiazole derivatives have been reported to possess potent anticancer activity. These substituted 1,3,4-oxadiazoles had shown different mechanism of action and participated in anticancer drug discovery and development. This review is complementary to earlier reviews and aims to review the work reported on anticancer activities of 1,3,4-oxadiazole derivatives from year 2000 to the beginning of 2020. K E Y W O R D S 1,3,4-oxadiazole, cancer, histone deacetylase, synthesis, tubulin polymerizations | 573 VAIDYA et Al. anticancer evaluation of 1,3,4-oxadiazole derivatives as inhibitors of Kinesin spindle protein (KSP). KSP inhibitors have been utilized for the treatment of inflammation, hyperplasias, cancer, and immune disorders. Furthermore, Shashikumar and colleagues in year 2015 obtained a WO (World intellectual property organization) patent for 1,3,4-oxadiazoles as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signaling pathway. Theses patented compounds having the ability to boost the immunity and were reported as immunomodulators. The growing patent literature of recent years demonstrates that the 1,3,4-oxadiazoles are becoming of great practical significance. The literature clearly reported numerous mechanism for anticancer activities of substituted 1,3,4-oxadiazole derivatives (Zhang et al., 2010, 2011). Recently, Glomb et al. (2018) published a notable review article, describing antiproliferative effects of 1,3,4-oxadiazoles associated with their numerous mechanisms, including inhibition of growth factors, enzymes, kinases and others. Irrespective of Glomb et al. (2018) review in which they were cited numerous anticancer mechanism of 1,3,4-oxadiazoles, herein we had focused on several 1,3,4-oxadiazole derivatives for their anticancer activity. Especially, we focus this review on in vitro and in vivo anticancer activities of 1,3,4-oxadiazoles in the perspective of cancer drug development and refinement.

1,3,4-Oxadiazole-naphthalene hybrids as potential VEGFR-2 inhibitors: design, synthesis, antiproliferative activity, apoptotic effect, and in silico studies

“…The 1,3,4-oxadiazole moiety has various biological activities. The wide and potent activity of this moiety made it an important pharmacological scaffold for drug design especially in the field of cancer disease 5 , 40 , 41 . Additionally, naphthalene is a main building block in many anticancer agents 42 , 43 .…”

Caspase‐3: A primary target for natural and synthetic compounds for cancer therapy

“…Many caspase‐3 activation‐mediated apoptosis inducers for potential cytotoxicity have been reported till date (Jain et al., 2012, 2013, 2019; Jain, Pattnaik, et al., 2017; Kumar et al., 2021; Lv et al., 2020; Vaidya et al., 2020a, 2020b; Vaidya, Pathak, et al., 2020). Numerous SAR and QSAR studies were reported in favor to search of these compounds (Mansouri et al., 2020; Jain, Vaidya, et al., 2017; Şenkardeş et al., 2021; Vaidya et al., 2014).…”

COVID-19 pandemic: The deadly respiratory disease of 21st century

“…Recently numbers of natural and synthetic drugs have been reported for symptomatic treatments. [20][21][22][23][24][25][26][27][28][29] Numerous drug design studies have been reported for search of novel compounds. [30][31][32][33][34][35][36][37][38] Numbers of novel drug delivery systems have been utilizes for effective drug delivery.…”