Science, Nature & Maths      Chemistry

Sintesi di (-) - pirenoforolo, valutazione antitumorale degli eterocicli: derivati di benzimidazolo, benzitiazolo e sulfonamide

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Book Details
Language
Italian
Publishers
Edizioni Sapienza (11 Jun. 2024)
Weight
0.18 KG
Publication Date
11/06/2024
ISBN-10
6207636112
Pages
112 pages
ISBN-13
9786207636112
Dimensions
15 x 0.66 x 22 cm
SKU
9786207636112
Author Name
PERUGU EDUKONDALU (Author)
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È stata realizzata la sintesi totale del (-)-pirenoforolo con elevata selettività enantio, in cui gli stereocentri sono stati stabiliti mediante risoluzione idrolitica cinetica di Jacobsen e la diidrossilazione asimmetrica Sharpless e la ciclizzazione è stata ottenuta mediante ciclizzazione intermolecolare di Mitsunobu. Il composto 90b con gruppo 3,4,5-trimetossi donatore di elettroni sull'anello fenilico, ha mostrato un'eccellente attività antitumorale (MCF-7 = 0.

018±0. 0039 μM, Colo-205 = 0.

12±0. 029 μM, Colo-205 = 0.

12±0. 029 μM, Colo-205 = 0.

17±0. 029 μM.

018±0,0039 μM, A549 = 0,011±0,0019 μM, Colo-205 = 0,12±0,029 μM e A2780 = 0,17±0,023 μM) rispetto all'etoposide. Il composto 117i, ricco di elettroni sulla parte fenilica, ha mostrato maggiori proprietà antitumorali su tutte le linee cellulari (PC3=0,11±0,068 μM; A549=0,18±0,063 μM; MCF-7= 0,52±0,074 μM e DU-145=0,17±0,082 μM).

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