A new isatin‐triazole tethered rhodamine based fluorescent probe R1 (1‐(2’’‐(4’‐(((3’’’,6’’’‐bis(diethylamino)‐3’’‐oxospiro[isoindoline‐1’’,9’’’‐xanthen]‐2’’‐yl)amino)methyl)‐1H‐1’,2’,3’‐triazolyl)ethyl)indoline‐2,3‐dione) has been synthesized using click chemistry approach. Probe R1 exhibits a dual sensor property for Cu2+ and Fe3+ ions through turn‐on fluorescence response. A prominent colour change from colourless to pink allows the naked eye identification of aforementioned metal ions. R1 forms a 1:2 complex with Cu2+ and Fe3+ ions with binding constants 8.0 × 108 and 2.93 × 107 M−2, respectively. The binding mode is scrutinised through various spectroscopic techniques which is further supported by theoretical calculations. The detection limit of R1 for Cu2+ and Fe3+ ions is found to be 12.2 nM and 0.33 μM, respectively. Further, R1 has been evaluated for its potential to detect Cu2+ ions in biological systems using fluorescence cell imaging studies.
A series of novel triazole linked isatin-dihydropyridine hybrids (N1-N15) have been synthesized and examined for their anti proliferative activity against human cancer cell lines viz. HeLa, Huh-7, PC-3, IMR-32 and MCF-7. All of the synthesized hybrids have shown moderate to potent cytotoxicity against all the tested cell lines except IMR-32. Compounds N1, N2 and N13 have displayed an enhanced inhibitory potency against Huh-7 cell line as compared to the standard drug, doxorubicin. Out of the three, N2 has shown the highest in vitro inhibitory action with IC 50 values of 6.73 � 0.33 μM and 17.94 � 0.23 μM against Huh-7 and MCF-7 cell lines, respectively. The docking studies of these most potent compounds have also been investigated which identified that N2 might be an excellent drug-like candidate worthy of further pursuit.
A novel pyranopyrazole-based Schiff base PPS has been synthesized via a condensation reaction between aldehyde and hydrazide derivatives of pyranopyrazole.
A glycerol-triazole tethered rhodamine based colorimetric and fluorimetric sensor 3',6'-bis(diethylamino)-2-(((1-(1,3-dihydroxypropan-2-yl)-1H-1,2,3-triazol-4-yl)methylene)aminospiro [isoindoline-1,9'-xanthen]-3-one (L1) is designed and synthesized for the selective recognition of Cu 2 + ion. The sensor L1 allows naked eye detection of Cu 2 + ion with a fast response (< 1 min). Among the various metal ions tested, the sensor L1 shows selective binding with Cu 2 + through turn-on fluorescence mechanism. The sensor shows 1 : 2 binding stoichiometry with binding constant, K a = 1.1 × 10 6 M À 2 as revealed by job's plot & Benesi-Hildebrand plot (BÀ H plot), respectively. The detection limit of L1 with Cu 2 + ion is found to be 3.3 μM. Further, the experimental results are also validated using density functional theoretical (DFT) study. The optimized geometries indicates that the formation of the L1-Cu 2 + complex is thermodynamically favourable by ΔG = À 11.7 kcal/mol. The HOMO-LUMO gap of the ligand L1 is found to be 3.49 eV, which decreases to 1.76 eV upon complexation with copper.
A series of novel 1-triazolylpyranopyrazole derivatives has been designed and synthesized using microwave irradiation, with the purpose of obtaining repositioned pharmaceutics. The newly synthesized 1-triazolylpyranopyrazoles (7 a-7 n), along with their precursor alkyne (5), have been screened for their invitro anti-tumor activity against Hep3B and HEK cell lines. The majority of triazolylpyranopyrazoles elicited outstanding anticancer activity on Hep3B cell lines even at concentrations as low as 25μg/mL. Further, molecular docking of these active compounds against Topoisomerase IIa substantiated a plausible target site for the compounds inhibiting Hep3B cells effectively. The biological assay results for the triazolylpyranopyrazole even surpassed the activity of the reference drug i. e. Doxorubicin, thereby appearing to be potent anticancer agents.
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