Library name

 Brief description

Arsenic, a known human carcinogen, can induce tumors of the skin, urinary bladder, liver and lung etc.. On the other hand, arsenic is also a novel promising anticancer agent, and can be used effectively to treat acute promyelocytic leukemia (APL) and some other tumors.

Aurora kinases are overexpressed in a variety of tumor cell lines, suggesting their potential role as cancer target for molecular therapies.

Aziridine analogues

Compound with aziridine substructure unit have potential anticancer activity.

BCL-2  inhibitors

(B-cell lymphoma 2)

BCL-2 family of proteins plays critical roles in human cancers,, suggesting that the discovery of specific agents targeting Bcl-2 family proteins would be extremely valuable for cancer therapy. 

BCR-ABL inhibitors

(Bcr-Abl tyrosine kinase inhibitors)

The BCR-ABL chimeric protein is thought to play a central role in the pathogenesis of Philadelphia (Ph) chromosome-positive leukemias, notably chronic myeloid leukemia (CML). BCR-ABL tyrosine kinase  may be suitable targets for  cancer therapy.

CA  inhibitors

(carbonic anhydrase)

Carbonic anhydrase inhibitors can selectively block the enzyme activity of cancer-related isoforms, namely CA IX and CA XII. Thus, CA inhibitors may have potential anticancer activity

Cell cycle checkpoint inhibitors

Cell cycle checkpoints are activated in response to DNA damage. Their role consists in blocking the cell cycle to allow time for DNA repair. Among the regulators of the G2 checkpoint, Checkpoint 1 kinase (Chk1) plays a major role. Chk1 inhibitors as potential useful compounds can enhance the antitumor efficiency of DNA damaging agents.

c-Met inhibitor

(mesenchymal-epithelial transition factor)

c-Met is a receptor tyrosine kinase that plays a key role in several cellular processes but has also been found to be overexpressed and mutated in different human cancers.  The c-MET inhibitor may have a significant therapeutic potential.

 Dual  kinase inhibitors

Dual receptor tyrosine kinase inhibitors includes:

VEGF/EGFR inhibitors; EGFR/ErbB-2 inhibitors; EGFR and HER2  inhibitors; ErbB1 (EGFR/HER1)  inhibitors, ErbB2 (HER2/neu) inhibitors,

 Farnesyl  transferase inhibitors

Farnesyl transferase inhibitors are a new class of biologically active anticancer drugs. The inhibition of farnesylation of a wide range of target proteins will ultimately result in cell growth arrest. 

 FLT3 inhibitors

(FMS-like tyrosine kinase 3)

FMS-like tyrosine kinase 3 (FLT3) is a receptor tyrosine kinase (TK) expressed by immature hematopoietic cells and is important for the normal development of stem cells and the immune system.

FLT3 inhibitors have some potential anticancer activity.

HDAC  inhibitors

(Histone deacetylase)

Histone deacetylases (HDACs) catalyze the removal of acetyl groups from histones and contribute to transcriptional repression.   HDAC inhibitors can induce cell-cycle arrest, promote differentiation, and stimulate tumor cell death.

Hypoxia cytotoxic agents

Hypoxia is associated with tumour hypoxia including: resistance to ionising radiation, resistance to chemotherapy and the magnification of mutated p53. As such this provides a significant target for drug discovery particularly for tumour-targeting agents.

IGF-IR inhibitors

(insulin-like growth factor receptor)

IGF-IR and insulin receptor contribute to tumorigenicity, proliferation, metastasis, and drug resistance. As IGF signaling has been recognized to play an important role in human cancer, the IGF-IR  is currently the focus of intensive research aimed at developing novel antitumor agents.

IMPDH  inhibitors

(Inosine Monophosphate Dehydrogenase )

IMPDH is the rate-limiting enzyme for de novo purine synthesis. Inhibition of IMPDH results in reduced levels of guanylates, resulting in the inhibition tumor cell growth in vitro and in vivo.

 JNK  inhibitors

(c-Jun-N-Terminal Kinase)

Inhibitors of c-Jun-N-Terminal Kinase (JNK) have many potential therapeutic indications ranging from neurodegenerative disease, to metabolic disorders, inflammation, cardiovascular disease, and cancer.  

KSP inhibitors

(Kinesin  spindle protein)

Kinesin spindle protein (KSP) plays a critical role in mitosis as it mediates centrosome separation and bipolar spindle assembly and maintenance. Inhibition of KSP function leads to cell cycle arrest at mitosis with the formation of monoastral microtubule arrays, and ultimately, to cell death.

 LTB4 receptor antagonists

(leukotriene B4  receptor)

The blockade of the LTB(4)-signaling pathway induces apoptosis via the inhibition of ERK activation in colon cancer cells. The LTB(4)-signaling pathway might be a new therapeutic target for colon cancer.

MGMT/AGT inhibitors

(O6-methylguanine DNA methyltransferase/O6-alkylguanine DNA alkyltransferase )

MGMT/AGT removes alkyl adducts from the O6-position of guanine in DNA. Expression of MGMT in human cancers has been associated with resistance to therapies using alkylating agents. MGMT/AGT inhibitors may enhance efficacy of alkylatin anticancer agents

 MMP  inhibitors

(atrix metalloproteinases)

The matrix metalloproteinases (MMPs) are involved in many aspects of both physiological cellular processes and pathological situations, such as tumor growth, invasion and metastasis. MMPs have been considered prognostic factors in various types of cancer as well as promising targets for cancer therapy.

NK1 receptor antagonists

(neurokinin-1 receptor antagonist) 

The presence of functional NK1 receptors has been documented in malignant brain tumours of glial origin.  It has been suggested that SP receptor antagonists application might be useful in attempts directed at anti-cancer therapy.

Nitrogen mustard

The nitrogen mustards are bifunctional alkylating agents which, although used extensively in cancer chemotherapy, are themselves highly carcinogenic

PARP inhibitors

(Poly (ADP-ribose) polymerase (PARP))

 PARP inhibition is associated with increased sensitivity to DNA-alkylating agents, topoisomerase I poisons and ionising radiation.

Phosphamide  mustard

Phosphamide  mustard belongs to alkylation agents.

 PLK-1  inhibitors

(polo-like kinase 1 )

PLK1 is overexpressed in human tumours and has prognostic potential in cancer, indicating its involvement in carcinogenesis and its potential as a therapeutic target.

Quinazoline Kinase inhibitors

4-anilinoquinazoline and its analogues  are potent and selective kinase inhibitors with potential anticancer activity.

SPR  modulators

(Selective progesterone receptor)

Selective progesterone receptor modulators (SPRMs) represent a new class of progesterone receptor ligands.  SPRMs have the potential to become a novel treatment of uterine fibroids, endometriosis and cancer.

 STAT 3 inhibitors

(Signal transducer and activator of transcription 3)

STAT-3  is constitutively activated by aberrant upstream tyrosine kinase activities in a broad spectrum of human tumors, and it has been identified as a promising target for cancer drug discovery.

STS inhibitors

(Steroid sulfatase)

STS  inhibitors are potential anticancer agents.

Survivin inhibitors

Survivin belongs to the inhibitor of apoptosis protein (IAP) family that acts as a suppressor of apoptosis and plays a central role in cell division. Survivin is currently undergoing extensive investigation as a novel therapeutic target

TS inhibitors

(Thymidylate synthase)

Thymidylate synthase (TS) is a well-validated target for cancer chemotherapy.

Vascular disrupting agents (VDAs)

Vascular disrupting agents (VDAs) are a new class of potential anticancer drugs that selectively destroy tumor vasculature and shutdown blood supply to solid tumors, causing extensive tumor cell necrosis.