Τίτλος:
Novel Substituted Purine Isosteres: Synthesis, Structure-Activity Relationships and Cytotoxic Activity Evaluation
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
A number of pyrrolo[2,3-c]pyridines, pyrrolo[3,2-d]pyrimidines and pyrazolo[4,3-d]pyrimidines were designed and synthesized as antiproliferative agents. The target compounds possessed selected substituents in analogous positions on the central scaffold that allowed the extraction of interesting SARs. The cytotoxic activity of the new derivatives was evaluated against prostatic (PC-3) and colon (HCT116) cell lines, and the most potent analogues showed IC50 values in the nM to low µM range, while they were found to be non-toxic against normal human fibroblasts (WI-38). Flow cytometric analysis of DNA content revealed that the most promising derivative 14b caused a statistically significant accumulation of PC-3 cells at G2 /M phase and induced apoptosis in PC-3 cells. © 2021 by the authors. Licensee MDPI, Basel, Switzerland.
Συγγραφείς:
Dimitrakis, S.
Gavriil, E.-S.
Pousias, A.
Lougiakis, N.
Marakos, P.
Pouli, N.
Gioti, K.
Tenta, R.
Λέξεις-κλειδιά:
antineoplastic agent; pyrimidine derivative, cell cycle; cell proliferation; chemical structure; chemistry; dose response; drug effect; fibroblast; human; metabolism; structure activity relation; synthesis; tumor cell line, Antineoplastic Agents; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Chemistry Techniques, Synthetic; Dose-Response Relationship, Drug; Fibroblasts; Humans; Molecular Structure; Pyrimidines; Structure-Activity Relationship
DOI:
10.3390/molecules27010247
