Design, synthesis, and biological evaluation of matrine derivatives possessing piperazine moiety as antitumor agents

Piperazine skeleton in the structural modification of natural products: a review

“…Compound 51a and 51b (Figure 26) showed strong antitumor activity against human hepatoma Bel-7402 and colorectal carcinoma RKO cells (IC 50 ¼ 50.4 ± 1.4 mM and 48.3 ± 3.1 mM, 48.3 ± 2.5 mM and 51.3 ± 3.3 mM, respectively), proved to be of much better therapeutic efficacy than parent compound matrine (IC 50 ¼ 86.6 ± 2.6 mM and 84.3 ± 2.5 mM, respectively) and positive control cisplatin (IC 50 ¼ 92.5 ± 1.6 mM and 68.0 ± 1.3 mM, respectively). The SAR analysis indicated that the introduction of a piperazine moiety on matrine might significantly improve its antiproliferative activity, and the substituents and their position on phenyl of R1 and the variation of R2 could take a great role in antitumor activity 78 .…”

Development of newly synthesised quinazolinone-based CDK2 inhibitors with potent efficacy against melanoma

“…In the course of finding several chemical substances which may serve as leads for developing new anticancer agents, we are particularly interested in the present study with quinazolinone derivatives in an attempt to achieve novel CDK2 inhibitors serving as chemotherapeutic agents. Continuing our studies on quinazolinone analogues as attractive candidates as antitumor agents 30 , 31 , we have designed some new quinazolinone derivatives containing phenoxy methyl group at position 2 and bearing different moieties which are known to enhance the antitumor activity attached to the 3-amino group viz un/substituted phenyl acetamides 32 , un/substituted benzene sulfonamides 33 , benzylidenes 34 , and acetyl piperazines 35 ( Figure 1 ). In this work, the substitution pattern at the 2 and 3 positions of the quinazolinone scaffold was selected to provide a different electronic environment that would affect the lipophilicity, and hence the activity of the target molecules.…”

Design, DFT Calculations and Antimicrobial Activity of New Synthesized Piperazine Derivative

“…The imine group (azomethine) of Schiff bases attracted much attention due to widely usage in biological studies and which was use in chemistry (Venkataramana et al, 2010;Yan et al, 2012;Gupta & Goklani, 2017;Ermiş & Durmuş, 2020). Piperazine ring is also an important class of N-heterocyclics having biological activities including antitumor (Xu et al, 2019), antiviral drugs (Hooshmand et al, 2021), antibacterial (Jalagari et al, 2019) and antifungal etc (Suryavanshi & Rathore, 2017) and pharmaceutical applications (Ullh et al, 2022). Piperazine derivatives have been widely used in the production of new drugs in recent years (Shaquiquzzaman et al, 2015).…”