KF-38789 is a selective inhibitor of P-selectin-mediated cell adhesion (IC50 = 1.97 uM) that displays no effects on L-selectin- and E-selectin-mediated adhesion. KF-38789 inhibits P-selectin-dependent cell adhesion, superoxide production by human PMN and TG-induced cell migration into the murine peritoneal cavity. It was also identified as a tubulin disruptor.

Epothilone A is a natural compound, originally discovered from the myxobacterium Sorangium cellulosum. Epothilones A, a macrolide compound, stabilizes polymerized microtubules, leading to mitotic arrest and cytotoxicity in proliferating cells. While epothilone A shows potent antineoplastic activity in vitro, these effects were not seen in preclinical in vivo models due to its poor metabolic stability and unfavorable pharmacokinetics.

4'-demethylepipodophyllotoxin (DMEP) belongs to the class of podophyllotoxin. Podophyllotoxin is a natural product from the roots and rhizomes of Podophyllum species and binds at the colchicine site as a microtubule inhibitor. DMEP is an antimitotic agent which binds to monomeric tubulin, preventing microtubule polymerization. It can reduce the tumor formation and growth in a mouse skin carcinogenesis model. DMEP derivatives exert strong antitumor properties.

PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.

Thiocolchicine is a colchicine-derivative used in the therapy of some diseases and extensively studied in the field of oncological research as antimitotic agent. It is tubulin polymerization and microtubule assembly inhibitor and axonal cytoskeleton modulator; apoptosis inducer. Thiocolchicine-dimers were shown to be potent topoisomerase I inhibitors. Thiocolchicine is a potential antitumor agent.

3,4,5-Trimethoxybenzaldehyde is a key intermediate in the synthesis of trimethoprim[2,4-diamino-5-(3,4,5-trimethoxybenzyl)pyrimidine], which, in addition to its antibacterial activity, possesses the property of significantly strengthening the bactericidal activity of sulfanilamide preparations. Also, 3,4,5-Trimethoxybenzaldehyde id used for the synthesis of Isoamoenylin, which showed moderate antioxidative and weak antibacterial activities. An A-ring analogue of colchicine, 3,4,5-trimethoxybenzaldehyde, can stop the antimitotic drug IKP104-induced unfolding of tubulin significantly. 3,4,5-trimethoxybenzaldehyde stimulated tubulin-dependent GTP hydrolysis.

Ansamitocin P3, a structural analogue of maytansine, was isolated from Nocardia. Structurally maytansine and ansamitocin P3 are polyketide macrolactams differing in the acyl groups at the C3 position. Ansamitocin P-3 inhibited the polymerization of tubulin and depolymerized the once polymerized tubulin. Ansamitocin P3 exerts antitumour properties.

gamma-sitosterol is a naturally occurring plant steroid isolatable from plants of the genus Lagerstroemia. Gamma-sitosterol is a potent inhibitor of the complement component C1 complex, and it has demonstrated potential as a diabetic treatment in rats. Gamma-sitosterol is a stereoisomer of beta-sitosterol, which sees wide use as an over the counter natural supplement. However, plant extracts containing gamma-sitosterol have demonstrated toxicity on in-vitro human cell assays; which may discourage use as a natural supplement.