Anticancer potential of fused heterocycles: structural insights and mechanistic advances

Aaysha Pandey; Shubham Sharma; Kamal Kishore; Swati Rani; Man Vir Singh; Gangotri Pemawat

doi:10.2478/abm-2025-0035

Figures & Tables

Selected anticancer derivatives of β-lactam derivatives, carbazoles, isatin derivatives, PBD, and pyrido[2,3-d]pyrimidine. PBDs, pyrrolo-benzodiazepines.

An image of C. guianensis (Abricó-de-macaco) tree.

A structure–activity relationship of isatin derivatives [40].

Structure of ellipticine, celiptium, and alectinib.

Structure of PBD core nucleus. PBDs, pyrrolo-benzodiazepines.

Few examples of PBD based biologically active compounds. PBDs, pyrrolo-benzodiazepines.

Binding mechanism of PBD with DNA. PBDs, pyrrolo-benzodiazepines.

PBD derivatives (1-3) as anticancer agents. PBDs, pyrrolo-benzodiazepines. Findings from the literature review suggest that PBD compounds have been examined for their potential anticancer properties and have demonstrated encouraging results in inhibiting the advancement of cancer cells.

Structure of pyrido[2,3-d]pyrimidine framework.

Examples of pyrido-pyrimidine based anticancer candidates.

Summary of anticancer agents

Type of compound	Compound name/structure	Activity	IC₅₀	Type of cancer cell/mechanism of action)
β -Lactams	N -Thiolated β -lactams	Anticancer	-	DNA
	4-Alkylidene β -lactams	Anticancer	-	Matrix metalloproteinases and leukocyte selections
Isatins	Sunitinib	Anticancer	-	ATP binding sites of kinases
	Toceranib	Anticancer and antitumor	-	Inhibitor of certain RTKs
	Amido/ureido-tethered isatin benzene sulfonamide hybrids	Anticancer	-	Block specific isoforms of carbonic anhydrase, particularly HCa IX and XII
	α, β-Unsaturated ketones generated from isatin	Anticancer	-	Reducing cell proliferation across several cancer cell lines
	Spirooxindole-derived morpholine-fused-1,2,3-triazoles	Anticancer	-	Antiproliferative effects against several cancer cell types
Carbazoles	Ellipticine	Anticancer	-	Inhibiting DNA synthesis and inducing programmed cell death in malignant cells
	Ceptium	Anticancer	-	Treatment of metastatic breast cancer since
	Alectinib	Anticancer	-	Target microtubules and inhibit tubulin assembly
	Anthramycins	Antitumor antibiotics	-	Selectively bind to DNA
PBDs		Anticancer	0.5–6.6 μM	HL-60, THP-1, U-937 and jurkat leukemia cell lines
		Anticancer	1.1–1.7 μM	Skin (A431), lung (A549), prostate (PC-3) and colon (HT-29)
		Anticancer	2.2 μM	Potent cytotoxicity against A375 cells
Pyrido[2,3-d] pyrimidines		Anticancer	0.02–0.86 μM	Cytotoxicity against HeLa, PANC1, MDA-MB-231, and A549 cell lines
		Anticancer	1.6–29.7 μM	SK-BR-3, BT-474, MCF-7, A549, and MDA-MB-231
		Anticancer	9.5–10.3 μM	Cytotoxicity against PC-3 cell lines
		Anticancer	0.3–9.6 μM	HCT-116, HepG-2, PC-3, and A549
		Anticancer	6.2 and 19.6 μM	MCF-7 and HepG2 cell lines
		Anticancer	3.0 and 10.5 μM	T-47D and MDA-MB-436

Anticancer potential of fused heterocycles: structural insights and mechanistic advances

Figures & Tables

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Summary of anticancer agents

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