4-Aminoquinazoline Analogs: A Novel Class of Anticancer Agents

Abstract

4-Aminoquinazoline analogs have been identified as a new class of cancer chemotherapeutic agents with significant therapeutic efficacy against solid tumors. They are potent and highly selective inhibitors of tyrosine kinase (TK) and epidermal growth factor receptor (EGFR). Till date various 4-aminoquinazoline analogs have been synthesized and evaluated for anticancer activity. This review is an attempt to compile the medicinal chemistry of various synthesized 4-aminoquinazoline analogs.

Epidermal Growth Factor Receptor Inhibiting 4‐Aminoquinazolines as Promising Anticancer Agents: A Patent Review (2000‐Present)

“…They have been recognized as another class of malignancy chemotherapeutic specialists with critical restorative adequacy against solid tumors. They are intense and exceedingly selective inhibitors of tyrosine kinase (TK) and epidermal development factor receptor (EGFR) [19,20] . A list of FDA‐approved kinase inhibitors and their drug targets are summarized in Table 1 [21] …”

“…They are intense and exceedingly selective inhibitors of tyrosine kinase (TK) and epidermal development factor receptor (EGFR). [19,20] A list of FDA-approved kinase inhibitors and their drug targets are summarized in Table 1. [21] Other coding that is used other than Table 1 that are usen in this review article.…”

Phosphatase CDC25B Inhibitors Produced by Basic Alumina-Supported One-Pot Gram-Scale Synthesis of Fluorinated 2-Alkylthio-4-aminoquinazolines Using Microwave Irradiation

“… 30 − 32 In particular, as one of the diverse quinazoline derivatives, 4-aminoquinazoline nucleus is commonly present in a variety of drug molecules and biologically active agents. 30 − 33 For example, gefitinib (Iressa) 34 , 35 and lapatinib (Tykerb) 36 have been extensively used as inhibitors of tyrosine kinases for the treatment of nonsmall cell lung cancer and breast cancer, respectively ( Figure 1 ). CCT241533 blocked checkpoint kinase 2 activity in human tumor cell lines in response to DNA damage ( Figure 1 ).…”

“…Quinazolines are an important class of N-containing heterocyclic compounds that have increasingly attracted considerable attention because of their diverse pharmacological activities, and they can be used as spinal muscular atrophy therapeutics, antiatrial fibrillation agents, anticancer drugs, − antimalarial agents, etc. − In particular, as one of the diverse quinazoline derivatives, 4-aminoquinazoline nucleus is commonly present in a variety of drug molecules and biologically active agents. − For example, gefitinib (Iressa) , and lapatinib (Tykerb) have been extensively used as inhibitors of tyrosine kinases for the treatment of nonsmall cell lung cancer and breast cancer, respectively (Figure ). CCT241533 blocked checkpoint kinase 2 activity in human tumor cell lines in response to DNA damage (Figure ).…”

Design, Synthesis and Structure-Activity Relationships of Novel Diaryl Urea Derivatives as Potential EGFR Inhibitors

“…Therein, thieno[3,2- d ]pyrimidine derivative S1 bearing diaryl urea moieties at the C-2 positon exhibited significant inhibition of tyrosine kinases, including c-Kit, orphan receptor tyrosine kinase (RET), and FLT3 for its prominent framework [9]. Similarly, the 4-aminoquinazolinyl skeleton, which competitively binds to the ATP binding pocket of intracellular kinase domains and blocks the conduction of downstream signaling networks mediated by tyrosine kinase, is also extensively used in the design of RTKs inhibitors (e.g., gefitinib, erlotinib and S2 ) [10,11].…”