Design, synthesis, and cytostatic activity of novel cyclic curcumin analogues

Effects of Different Carboxylic Ester Spacers on Chemical Stability, Release Characteristics, and Anticancer Activity of Mono-PEGylated Curcumin Conjugates

“…[13][14][15] Several approaches to enhance the water solubility, chemical stability, and resultant bioavailability of curcumin have been investigated. [16][17][18][19][20][21][22][23][24][25][26][27][28] Adding adjuvants such as piperine, which can inhibit glucuronidation metabolic pathways of curcumin, has been used to improve curcumin bioavailability. 16 Development of curcumin formulations as nanoparticles, liposomes, micelles, and phospholipid complexes is an alternative approach to prolong half-life, improve membrane permeability, and increase the metabolic stability of curcumin.…”

“…[17][18][19][20][21] A chemical modification approach has been used to generate curcumin derivatives with increased biological activity and improved pharmacokinetic properties. [22][23][24][25][26][27][28] For example, Qiu et al 26 synthesized a series of curcumin derivatives by replacing a phenyl ring with furan, and these compounds have higher inhibitory potency than curcumin against growth of several thioredoxin reductase-overexpressing cancer cell lines in vitro. Ferrari et al 27 synthesized glycosylated curcumin analogues with increased water solubility and improved stability, which resulted in higher cytotoxicity against a cisplatin-resistant human ovarian carcinoma cell line.…”

Kurkumin ve analoglarının antikanserojen etkileri

“…Kurkuminin iyi bir anti-neoplastik aktiviteye sahip olması, molekül ağırlığının düşük olması ve toksisitesinin olmaması, bu molekülü; potansiyel kemoterapötik bir bileşik geliştirilmesinde ideal öncü molekül haline getirmektedir [103,24]. Michael akseptörü olduğu için, protein tiyolasyonu yapabilmektedir [4]. Bu tür bileşiklerin sülfhidril grubu taşıyan topoizomeraz-2 gibi proteinlerle kovalent bağ yaparak enzimi inaktif hale getirdiği bilinmektedir [104].…”

“…Bu üç bileşiğin, diğer neoplastik hastalıklara oranla lösemide daha fazla toksisite gösterdiği sonucuna ulaşılmıştır [115]. 2-ariliden-5-(1-hidroksi-3-arilalliliden) siklopentanon ve 2-ariliden-5-(1-hidroksi-3-arilalliliden)-sikloheksanon bileşikleri seçici toksisite gösterebilen antikanser bileşiklere aday olarak önerilebilir [4].…”

Perspectives on New Synthetic Curcumin Analogs and their Potential Anticancer Properties

“…Youssef et al [60] prepared a series of novel analogues of curcumin, and analyzed their cytotoxic activity against L1210 (murine leukemia) and human lymphoblast Molt4C/8 CEM cell lines where compounds 54-57 were found to be cytostatic. Vyas et al [61] conjugated curcumin with a recombinant chimeric antibody cPiPP (58), exhibiting high affinity and specificity for human chorionic gona-dotropin-(hCG-)/hCG, which was tested for growth inhibitory properties against MOLT-4 and U-937 cells.…”