| Autor: |
Reddy, P. O. Venkataramana, Shekar, K. P. Chandra, Khandagale, Santosh B., Hara, Daiki, Son, Aoi, Ito, Takeo, Tanabe, Kazuhito, Kumar, Dalip |
| Předmět: |
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| Zdroj: |
Asian Journal of Organic Chemistry; Feb2019, Vol. 8 Issue 2, p269-274, 6p |
| Abstrakt: |
Microwave (MW)‐assisted efficient and rapid approach is developed to prepare water‐soluble cationic porphyrin‐β‐carboline conjugates by coupling of β‐carboline acid and 5‐(4‐aminophenyl)tripyridyl porphyrin and followed by N‐methylation of neutral porphyrin‐β‐carboline conjugates. Prepared neutral and cationic conjugates were screened for photocytotoxicity against lung (A549) and colon (Colon‐26) cancer cells. Conjugate 9 b was found to be the most potent conjugate with IC50 values ranging 39–47 nM against the tested cancer cell lines. Further, UV‐visible spectroscopy studies demonstrated that the conjugate 9 b in the presence of visible light shows intercalation upon binding to double‐stranded DNA. Additionally, the porphyrin‐β‐carboline conjugate 9 b (2.3×106 M−1) having binding constant (Kb) similar to H2TMPyP (2.5×106 M−1) displayed efficient visible light‐induced DNA cleavage and triggered cell death of A549 cells. A facile and efficient synthesis for water‐soluble cationic porphyrin‐β‐carboline conjugate 9 b endowed with remarkable photocytotoxicity (IC50∼39–47.7 nM) has been developed. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
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