Which are alkylating agents?

Some examples of alkylating agents are nitrogen mustards (chlorambucil and cyclophosphamide), cisplatin, nitrosoureas (carmustine, lomustine, and semustine), alkylsulfonates (busulfan), ethyleneimines (thiotepa), and triazines (dacarbazine).

What is the meaning of alkylating?

: the act or process of introducing one or more alkyl groups into a compound (as to increase octane number in a motor fuel)

What makes an alkylating agent?

What are Alkylating agents? Alkylating agents are compounds that work by adding an alkyl group to the guanine base of the DNA molecule, preventing the strands of the double helix from linking as they should. This causes breakage of the DNA strands, affecting the ability of the cancer cell to multiply.

What are alkylating agents in medicinal chemistry?

The alkylating agents are compounds that react with electron-rich atoms in biologic molecules to form covalent bonds. Traditionally, these agents are divided into two types: those that react directly with biologic molecules and those that form a reactive intermediate, which then reacts with the biologic molecules.

What are examples of alkylating agent?

Examples of alkylating agents include:

What are the classical alkylating agents?

Alkylating agents in the classic family include nitrogen mustard, cyclophosphamide, chlorambucil, melphalan, busulfan, and ifosfamide.

How do alkylating agents cause mutations?

Mutagenicity is related to the ability of alkylating agents to form crosslinks and/or transfer an alkyl group to form monoadducts in DNA. The most frequent location of adducts in the DNA is at guanines. Expressed mutations involve different base substitutions, including all types of transitions and transversions.

What are alkylation agents explain with reaction?

Alkylating agents are typically olefin, alcohols, sulfates halides and various nitrogen containing compounds that promote alkylation by enabling alkyl groups to selectively bond to molecules. Often, alkylation requires a catalyst. Common alkylating catalysts are acids, such as HF or H2SO4.

What are antimetabolite drugs?

Antimetabolites are a form of chemotherapy drug. They’re one of the most commonly used therapies to treat cancer. And they’re one of the oldest, dating back to the 1940s, when doctors used a medication that’s now considered an antimetabolite to treat children with leukemia.

What do alkylating agents do quizlet?

What do alkylating agents do? Attaches an alkyl group to DNA causing intra/inter-strand cross-linking. Can also modify the structure of guanine and cause ‘depurination’ – excision of the guanine.

Is bleomycin an alkylating agent?

DNA-damaging agents are among the most effective anticancer agents in clinical use; these include alkylating agents (e.g., cyclophosphamide, cisplatin), antimetabolites (e.g., 5-fluorouracil), topoisomerase inhibitors (e.g., etoposide), and cytotoxic antibiotics (e.g., bleomycin) [16].

Which of the following best describes the mechanism of action for alkylating agents?

Which of the following terms best describes its mechanism of action? Proflavine acts as an intercalating agent with DNA and binds using van der Waals interactions and ionic bonds. Alkylating agents react with DNA and form covalent bonds. … Busulfan acts as an alkylating agent.

Is Cytoxan an alkylating agent?

Cyclophosphamide is classified as an alkylating agent. Alkylating agents are most active in the resting phase of the cell. These drugs are cell-cycle non-specific.

What chemical reaction do alkylating agents participate in?

The alkylating agents are a group of strong disinfecting chemicals that act by replacing a hydrogen atom within a molecule with an alkyl group (CnH2n + 1), thereby inactivating enzymes and nucleic acids (Figure 13.3.

Why do alkylating agents have short half lives?

As noted above, alkylating agents generally have low TIs, because they target all dividing cells. Individual drugs have additional toxicities.

Is busulfan an alkylating agent?

Busulfan is a medication used in the management and treatment of allogeneic hematopoietic progenitor cell transplantation specifically for patients with chronic myelogenous leukemia. It is in the antineoplastic class of drugs. It is defined as an alkylating agent.

What is the mechanism of action of alkylating agents?

Most alkylating agents have similar mechanisms of action, but differ in their clinical efficacy. These agents act directly on DNA, resulting in its crosslinking and causing DNA strand breaks, leading to abnormal base pairing and inhibiting cell division, eventually resulting in cell death.

How alkylating agents cause leukemia?

Alkylating Agent–Induced Leukemias Alkylating agents induce dose-limiting myelosuppression and cause sublethal DNA damage to hematopoietic progenitors, causing mutational events that lead to malignant transformation to preleukemic and leukemic states.

Is cisplatin an alkylating agent?

Cisplatin is classified as an alkylating agent. Alkylating agents are most active in the resting phase of the cell.

What is a bifunctional alkylating agent?

Bifunctional alkylating agents form covalent bonds at two nucleophilic sites on different DNA bases to induce interstrand (between two opposite strands) and/or intrastrand (on same strand) cross-links (Fig. … Monofunctional agents have only one alkylating group and, therefore, cannot form crosslinks (Siddik, 2002).

Is Taxol an alkylating agent?

The three most active types of agents in the treatment of cancer of the ovary are platinum compounds (cisplatin or carboplatin), bifunctional alkylating agents (cyclophosphamide, melphalan, etc), and the recently developed natural product paclitaxel (Taxol; Bristol-Myers Squibb Company, Princeton, NJ).

Are alkylating agents mutagens?

The most commonly used chemical mutagens are alkylating agents such as ethylmethane sulfonate and N-methyl-N-nitrosourea that induce point mutations in DNA.

Can cells overcome the effects of alkylating agents?

Selected Alkylating Agents Can Overcome Drug Tolerance of G 0-like Tumor Cells and Eradicate BRCA1-Deficient Mammary Tumors in Mice. Clin Cancer Res.

Do alkylating agents cause DNA damage?

Alkylating agents constitute a major class of frontline chemotherapeutic drugs that inflict cytotoxic DNA damage as their main mode of action, in addition to collateral mutagenic damage.

Is Methotrexate an alkylating agent?

Cyclophosphamide, azathioprine, chlorambucil, and methotrexate are cytotoxic drugs used most commonly for the purpose of immunosuppression. Cyclophosphamide and chlorambucil are alkylating agents, which cause cross-linking of DNA resulting in altered protein production, decreased cell division, and cell death.

Which anticancer drug is an alkylating agent?

Cyclophosphamide — the most widely used alkylating agent of modern times.

Is thioguanine an alkylating agent?

Thioguanine is an antimetabolite in the synthesis of guanine nucleotides. 6) Alkylating Agents: Alkylating agents involve reactions with guanine in DNA. These drugs add methyl or other alkyl groups onto molecules where they do not belong.

What are metabolites?

Listen to pronunciation. (meh-TA-boh-lite) A substance made or used when the body breaks down food, drugs or chemicals, or its own tissue (for example, fat or muscle tissue).

What are called antimetabolites?

Antimetabolites are a class of anticancer drugs defined as compounds, structurally similar to natural purine or pyrimidine base, nucleoside or nucleotides, molecules needed to carry out primary metabolic reactions that by virtue of their similarity act as analogues of a normal metabolites, interfere with the normal …

Which antimicrobial agent is classified as an antimetabolite?

Sulfonamides and trimethoprim are examples of antimetabolites that interfere in the bacterial synthesis of folic acid by blocking purine and pyrimidine biosynthesis, thus inhibiting bacterial growth.