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A series of novel naphthoquinone-fused podophyllotoxins containing fluoro and trifluoromethyl substituents were synthesized in a medium with good yields using two different synthetic approaches: microwave-assisted four-component reactions of 2-hydroxy-1,4-naphthoquinone, tetronic acid, fluorinated arylaldehydes, and ammonium acetate, and microwave-assisted three-component reactions of 2-amino-1,4-naphthoquinone, tetronic acid, and fluorinated arylaldehydes. The structures of all products were confirmed by spectral analysis. Together, cytotoxicity assessment of the products against four human cancer cell lines (human carcinoma [KB], human hepatocellular carcinoma [HepG2], lung cancer [A549], breast carcinoma [MCF7], and human embryonic kidney [Hek-293]) was performed by MTT assay. Among the obtained compounds, compound 7f turned out to be the most potent anticancer agent with significant cytotoxic activity against KB, HepG2, and MCF cancer cell lines.

The anti-cancer activity of bannaxanthone E isolated from Garcinia mckeaniana leaves was assessed through a flow cytometric method on human lung SK-LU-1 cancer cells, including cell cycle changes and induction of cell apoptosis. Treatment with bannaxanthone E led to the suppression of cell cycle progression at the G2/M phase to 19.6% at 4 µM, and induced apoptosis via cell morphological changes, increased the fluorescence signal in caspase-3/7 activation, and accumulation of apoptotic cells in the SK-LU-1 line at 4 µM to 25.7%.

A new benzofurane 7-methoxy-2-(3-hydroxy-4-methoxyphenyl)-benzofuran-5-carboxylate (1) and 5 known compounds, such as propacin (2), hisbiscolatone A (3), heliclactone (4), rosmarinic acid (5), and syringaldehyde (6), were isolated from methanol extract of the Helicteres hirsuta stems. Their structures were elucidated by spectroscopic analysis as Nuclear Magnetic Resonance (NMR) and Mass Spectroscopy (MS) Furthermore, compounds 1 to 6 were evaluated for their cytotoxic activity against 4 human cancer cell lines such as Lu-1, MCF7, HepG2, and KB. The results showed that compound 2 exhibited moderate cytotoxic activity against Lu-1, MCF7, HepG2, and KB cell lines with IC50 values of 43.97 ± 2.12, 46.53 ± 0.75, 52.63 ± 0.24, and 56.37 ± 1.04 µg/mL, respectively. This is the first report of compounds 2 to 6 from H. hirsuta.

In order to find out the influence of carboxylic acid functionalities in the N-lactam side chains of indenoisoquinolines on cytotoxic activities, several new compounds have been synthesized and structurally characterized by analytical and spectral methods. The incorporation of a carboxylic acid group into the lactam side chain of indenoisoquinolines results in differences in cytotoxicity. The results indicated that compound 18c displayed substantial cytotoxic specificity toward KB and HepG2 cancer cells.

A series of 4-anilinoquinazoline–triazole–AZT hybrids were designed and synthesized as anticancer agents. Their cytotoxic potential has been evaluated by means of a micro-dilution assay against three human cancer cell lines (KB, epidermoid carcinoma; HepG2, hepatoma carcinoma; SK-Lu-1, non-small lung cancer). The biological results revealed that compounds 4b and 6d showed good anticancer activities against KB, HepG2, and Lu cell lines (IC50 values ranging from 9 μM to 100 μM). Especially, compounds 4b and 6d exhibited up to 3-fold more potent than reference drugs erlotinib hydrochloride and AZT in term of anti-lung cancer activity.

Series of novel artemisinin derivatives were designed and synthesized in which the amino propanol group was bonded to the artemisinin nucleus through C-C linkage. Ten new compounds were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity in KB and HepG2 cancer cell lines.