. Author manuscript; available in PMC: 2017 Dec 1.

Published in final edited form as: Bioorg Med Chem Lett. 2016 Oct 24;26(23):5703–5706. doi: 10.1016/j.bmcl.2016.10.063

Table 1.

Indolyl-tetralone chalcone derivatives produced via Scheme 1 and their cytotoxicity in A549 cancer cell line


Entry	Code	R¹	R²	R³	EC₅₀ (μM) (% of apoptotic cells at 10 μM) ^a
	1a	H	H	H	1.13
	1b	H	H	CH₃	0.47
	1c	H	H	C₂H₅	0.46
	2a	H	H	CH₃	0.47
	1d	H	H	BOC	(N.A.) ^b
	1e	F	H	CH₃	0.20
	1f	F	H	H	0.27
	1g	F	H	C₂H₅	0.11
	1h	F	H	CH₃CO	(28)
	1i	F	H	BOC	(N.A.)
	1j	F	H	Bn	(N.A.)
	1k	CH₃O	H	C₂H₅	3.0
	1l	CH₃O	H	H	0.55
	1m	CH₃O	H	CH₃	3.0
	2b	CH₃O	H	CH₃	5.8
	1n	CH₃O	CH₃O	CH₃	(N.A.)
	1o	CH₃O	CH₃O	C₂H₅	(19)
	2c	CH₃O	CH₃O	CH₃	10
	1p	Br	H	H	(16)
	1q	Br	H	CH₃	(21)
	2d	Br	H	CH₃	(26)
	1r	Br	H	C₂H₅	(N.A.)

average of triplicates, % of apoptotic cells in treatment groups as compared to DMSO controls.

N.A.: not active at 10 μM; Bn: benzyl; BOC: t-butoxycarbonyl. Docetaxel was used as a positive control and consistent with our historic results.