Scopus
Synthesis of New Picolylamine Bearing Calix[8]arene Derivatives as Antiproliferative Agents for Colorectal Carcinoma
ChemistrySelect · Ekim 2020
Makale Bilgileri
DergiChemistrySelect
Yayın TarihiEkim 2020
Cilt / Sayfa5 · 12250-12254
Scopus ID2-s2.0-85093871769
Özet
Calixarene macromolecules have been developed as essential candidate in pharmaceutical application as drug carrier. Possible functionalization with different small molecules at lower and upper rims uplifts biological activity in its structure. This work explain the application of lower rim-functionalized 4-picolylamine-calix[8]arenes (O-1 b and O-2 b) in antiproliferative potentials of several human cancerous cells (DLD-1, HT-29, MDA-231, and PC-3) as well as healthy epithelium cell (PNT1 A). The death mechanism and DNA interaction of O-1 b and O-2 b were also investigated. Syntheses of 4-picolylamine-calix[8]arenes (O-1 b and O-2 b) confirmed with different spectroscopic techniques including 1H NMR, 13C NMR, elemental analysis and FTIR. Results demonstrated that O-1 b and O-2 b compounds dose-dependently inhibited proliferation of DLD-1, HT-29, MDA-231, and PC-3 cells. The highest cytotoxicity was observed on colorectal carcinoma cells; DLD-1 with an IC50 value as 4.96 μM and 6.12 μM, respectively. These compounds were weak inhibitors on human healthy epithelium (PNT1 A) cells, while they significantly increased the apoptosis by interacting DNA molecule in a different manner. This is the first study to clarify the molecular mechanism of 4-picolylamine derived calix[8]arene on human cancerous cells.
Yazarlar (4)
1
Mehmet Oguz
2
Alev Gul
3
Serdar Karakurt
4
Mustafa Yilmaz
Anahtar Kelimeler
Apoptosis
Calix[8]arene
Comet Assay
Cytotoxicity
Picolylamine
Kurumlar
Selçuk Üniversitesi
Selçuklu Turkey
Metrikler
6
Atıf
4
Yazar
5
Anahtar Kelime