Efficient One-Pot Synthesis of Novel Caffeic Acid Derivatives as Potential Antimalarials

Table 3

The antimalarial activity of the series of novel derivatives of caffeic acid against the D10 (CQ-sensitive) and W2 (CQ-resistant) strains of P. falciparum and their cytotoxicity to NHDF cells.

Compound	P. falciparum IC50 (μM)		RI^a	Cytotoxicity^b IC50 (μM)	SID10^c	SIW2^d
	D10	W2
1			3.02		8.73	2.89
2			0.92		2.74	2.98
3			0.89		6.23	7.02
4			0.90		7.42	8.24
5			0.90	nd^e	—	—
6			0.91		1.77	1.95
CA	>277.53	>277.53	—	nd^e	—	—
CQ			11.5	^f	2047.5	178.04

^aRatio between the IC₅₀ values of each compound against the W2 and D10 strains of P. falciparum. ^bThe cytotoxic activity assayed in vitro on NHDF cells using the MTT assay. ^c. ^d4 SIW2 IC50 (NHDF)/IC₅₀ (W2). ^eNot determined. ^fData taken from reference [33].