Identification of novel anti-cancer agents by the synthesis and cellular screening of a noscapine-based library

Role of motor proteins in human cancers

“…Noscapine, which is a natural compound with anticancer properties, was shown to target MT. Novel synthetic noscapine derivatives were of much higher potency, showing promising results in preliminary studies ( Nemati et al, 2021 ) .…”

An Overview of Natural and Synthetic Phthalides Involved in Cancer Studies: Past, Present, and Future

“…Phthalide derivatives have been attracted interest as promising anticancer drug candidates to improve the therapeutic effect by site-specific administration or site-specific drug activation in advanced preclinical and clinical trials. [161][162][163][164][165] Noscapine (2), [36,37,40,126,127,130,132,148,161,[165][166][167][168][169][170][171][172][173][174][175][176][177] 3-n-butylphthalide (NBP) (6), [138,[178][179][180][181] mycophenolic acid (MPA) (13), [163,[182][183][184][185][186][187][188] mycophenolate mofetil (MMF) (14) (the morpholino ethyl ester prodrug of 13) [162,[189][190][191] are some of the good examples of those phthalide analogs that have been investigated and proposed for the treatment of cancer (Figure 2 and Figure…”

“…Olaparib (Lynparza by AstraZeneca), which is a poly ADP ribose polymerase (PARP) enzyme inhibitor playing role in DNA repair is one of the European Medicines Agency (EMA) and FDA approved drugs built by use of phthalide for the treatment of some cancers [40] such as; advanced ovarian, breast, and prostate. Mycophenolic acid (13), used as an immunosuppressant in kidney transplantation, [30,182,197] is another FDA approved drug phthalide analog.…”

“…Phthalide derivatives have been attracted interest as promising anticancer drug candidates to improve the therapeutic effect by site‐specific administration or site‐specific drug activation in advanced preclinical and clinical trials [161–165] . Noscapine ( 2 ), [36,37,40,126,127,130,132,148,161,165–177] 3‐n‐butylphthalide (NBP) ( 6 ), [138,178–181] mycophenolic acid (MPA) ( 13 ), [163,182–188] mycophenolate mofetil (MMF) ( 14 ) (the morpholino ethyl ester prodrug of 13 ) [162,189–191] are some of the good examples of those phthalide analogs that have been investigated and proposed for the treatment of cancer (Figure 2 and Figure 3). Phthalides are also the key intermediates [2] and they play a role as building blocks in the synthesis of natural products, such as fuscinarin [192] which is a human CCR5 antagonist used to block the entry of HIV into the host cells.…”

“…Noscapine ( 2 ) is one of the good examples of phthalide analogs with tubulin‐binding action [161,165,168,170,173] . Its antitumor activity has been demonstrated in several in vivo and in vitro studies [36,37,40,126,127,130,132,148,161,165–167,169–172,174–177] . Anticancer properties of noscapine through microtubule dynamics [170,173,175] are based on the binding ability of noscapine to tubulin which is a heterodimeric guanine nucleotide‐binding protein [132,161] .…”